Article
Mutations within the cholecystokinin-B/gastrin receptor ligand 'pocket' interconvert the functions of nonpeptide agonists and antagonists.
Molecular pharmacology - 1 Nov 1998
Bläker M, Ren Y, Gordon M C, Hsu J E, Beinborn M, Kopin A S
Abstract excerpt
We have reported previously that the transmembrane domains of the cholecystokinin-B/gastrin receptor (CCK-BR) comprise a putative ligand binding pocket. In the present study, we examined whether amino acid substitutions within the CCK-BR pocket altered the affinities and/or functional activities of L-365,260 (the prototypical nonpeptide CCK-BR antagonist) and two structural derivatives, YM022 (a higher affinity...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
